Nelociguat-BAY60-4552-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENelociguatCat. No.: HY-78237CAS No.: 625115-52-8Synonyms: BAY60-4552分式: CHFNO分量: 408.39作靶點(diǎn): Guanylate Cyclase作通路: GPCR/G Protein儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 105 mg/mL (25

2、7.11 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.4486 mL 12.2432 mL 24.4864 mL5 mM 0.4897 mL 2.4486 mL 4.8973 mL10 mM 0.2449 mL 1.2243 mL 2.4486 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使

3、；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.67 mg/mL (6.54 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.67 mg/mL (6.54 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBI

4、OLOGICAL ACTIVITY物活性 Nelociguat (BAY60-4552)種氧化氮敏感的可溶性的鳥(niǎo)苷酸環(huán)化酶激活物。體外研究 Soluble guanylate cyclase (sGC) is a key enzyme in the nitric oxide (NO) signalling pathway 1. Riociguat ismetabolized to BAY60-4552 not only via cytochrome P450 isoenzymes 3A4 (CYP3A4), CYP2C8, andCYP2J2, but also via CYP1A1, loc

5、ated in the liver and lungs 2.體內(nèi)研究 GSK2181236A and BAY 60-4552 provide partial benefit against hypertension-induced end-organ damage. Inspontaneously hypertensive stroke-prone rats, a low dose of BAY 60-4552 decreases urine output andimproved survival. A high dose also reduces urine output, and in a

6、ddition reduces microalbuminuria andattenuates the increase in mean arterial pressure. Both the 0.3 and 3 mg/kg/day doses of BAY 60-4552improves survival of 46 and 69%. Seven weeks of treatment with BAY 60-4552 (0.3 and 3.0 mg/kg/day)dose-dependently decreases urine output to 7911 and 5610 mL/day 1.

7、 BAY 60-4552, and vardenafilprovides synergistic beneficial effects and might therefore salvage patients who experience treatment failureswith PDE5 inhibitors after radical prostatectomy 3.PROTOCOLAnimal Rats: Rats are orally gavaged with vehicle (0.5% HPMC, 5% DMSO, and 0.1% Tween 80; 10 mL/kg; n=1

8、4),Administration 1 GSK2181236A (0.1 or 1.0 mg/kg; n=11-14), or BAY 60-4552 (0.3 or 3.0 mg/kg; n=10-12) 2 h prior toischemia. Blood is collected at the initiation of ischemia and after 24 h reperfusion. Plasma is obtained foranalysis 1.MCE has not independently confirmed the accuracy of these method

9、s. They are for reference only.REFERENCES1. Costell MH, et al. Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associatedwith oxidative stress. Front Pharmacol. 2012 Jul 5;3:128.2. Zhao X, et al. Pharmacokinetics of the Soluble Guanylate Cyclase

10、 Stimulator Riociguat in Healthy Young Chinese Male Non-Smokersand Smokers: Results of a Randomized, Double-Blind, Placebo-Controlled Study. Clin Pharmacokinet. 2016 May;55(5):615-24.3. Oudot A, et al. Combination of BAY 60-4552 and vardenafil exerts proerectile facilitator effects in rats with cavernous nerve injury: aproof of concept study for the treatment of phosphodiesterase type 5 inhibitor failure. Eur Urol. 2011 Nov;60(5):1020-6.McePdfHeightCaution: Product has not been ful